Total synthesis of 6-deoxypladienolide D and Assessment of Splicing Inhibitory Activity in a Mutant SF3B1 cancer cell line.
Org Lett
; 16(21): 5560-3, 2014 Nov 07.
Article
in En
| MEDLINE
| ID: mdl-25376106
ABSTRACT
A total synthesis of the natural product 6-deoxypladienolide D (1) has been achieved. Two noteworthy attributes of the synthesis are (1) a late-stage allylic oxidation which proceeds with full chemo-, regio-, and diastereoselectivity and (2) the development of a scalable and cost-effective synthetic route to support drug discovery efforts. 6-Deoxypladienolide D (1) demonstrates potent growth inhibition in a mutant SF3B1 cancer cell line, high binding affinity to the SF3b complex, and inhibition of pre-mRNA splicing.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Phosphoproteins
/
RNA Splicing
/
Ribonucleoprotein, U2 Small Nuclear
/
Macrolides
/
Cell Line, Tumor
/
Cell Proliferation
/
Epoxy Compounds
/
Antineoplastic Agents
Limits:
Humans
Language:
En
Journal:
Org Lett
Journal subject:
BIOQUIMICA
Year:
2014
Document type:
Article
Affiliation country:
United States